2. Academic Validation
  3. Conformationally restricted analogs of Combretastatin A-4 derived from SU5416

Conformationally restricted analogs of Combretastatin A-4 derived from SU5416

  • Bioorg Med Chem Lett. 2005 Dec 15;15(24):5382-5. doi: 10.1016/j.bmcl.2005.09.001.
Pui-Kai Li 1,  Zili Xiao,  Zhigen Hu,  Bulbul Pandit,  Yanjun Sun,  Dan L Sackett,  Karl Werbovetz,  Andrew Lewis,  Jayasekar Johnsamuel
Affiliations

Affiliation

  • 1 Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA. li.27@osu.edu
PMID: 16213720 DOI: 10.1016/j.bmcl.2005.09.001
Abstract

A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, was synthesized and evaluated. The most potent compound in this series, compound 7, structurally resembles the potent anti-microtubule agent Combretastatin A-4, inhibited tubulin polymerization, and showed potent growth inhibitory activities on both prostate and breast Cancer lines with IC(50) values in low to subnanomolar range.

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